Topical Triterpene Composition for Stable Dermal Delivery
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Solution Overview
Problem
Existing formulations struggle to deliver and stabilize poorly water-soluble biologically active substances like pentacyclic triterpenes through the skin, leading to instability and reduced bioavailability.
Innovation Solution
A composition combining poly-n-glyceryl-sorbityl enoxolone with highly branched cyclic dextrin is used to create a stable topical delivery and release system for pentacyclic triterpenes, enhancing solubility and bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If traditional cyclodextrins or liposomal systems are used to deliver pentacyclic triterpenes, then solubility and bioavailability are improved, but stability in formulations containing ethyl alcohol or amphiphilic substances deteriorates
Solution Approach 1:
The patent modifies the cyclodextrin structure by introducing hydrophobic substituents at the C6 position of glucose units, changing the physical-chemical parameters of the carrier to improve compatibility with lipophilic active substances and alcohol-based formulations, thereby resolving the contradiction between bioavailability enhancement and formulation stability
Solution Approach 2:
The invention creates a composite system combining modified cyclodextrin with specific carriers (water, oils, waxes, alcohols, gels) to form stable formulations that maintain both the delivery efficiency for pentacyclic triterpenes and compatibility with cosmetic/pharmaceutical ingredients, particularly ethyl alcohol and amphiphilic substances
2Reliability
If liposomes or niosomes are used as release systems, then dermal absorption is facilitated, but instability occurs in the presence of protic polar solvents like ethyl alcohol
Solution Approach 1:
The patent replaces unstable liposomal/niosomal systems with modified cyclodextrin inclusion complexes that are chemically more stable in alcohol-containing formulations, sacrificing some of the vesicle-specific benefits for overall formulation stability and compatibility with cosmetic ingredients
Solution Approach 2:
By modifying the cyclodextrin structure with hydrophobic groups, the patent changes the solubility and stability parameters of the release system, enabling it to maintain structural integrity in the presence of ethyl alcohol and amphiphilic substances while still facilitating dermal absorption
3Reliability
If amphiphilic substances are added to improve solubility of pentacyclic triterpenes, then bioavailability increases, but structural integrity of vesicles deteriorates
Solution Approach 1:
The modified cyclodextrin acts as an intermediary carrier that solubilizes pentacyclic triterpenes through inclusion complexation without requiring additional amphiphilic substances, thereby maintaining the structural integrity of the release system while achieving the desired solubility enhancement
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The system effectively delivers and modulates the release of pentacyclic triterpenes, improving bioavailability and stability, suitable for cosmetic and pharmaceutical applications.
Implementation Method 1
Cyclodextrins have the ability to form solid inclusion complexes (host-guest complexes) with host compounds via molecular complexation. In these complexes a guest molecule is positioned inside the cavity of the cyclodextrin host.
Implementation Method 2
The systems to topically release active substances are formulated in such a way as to deliver the active substances through the epidermis and regulate the release rate of these active substances.
Data Source
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AI summary
The invention relates to a system or composition to topically deliver and/or release a pentacyclic triterpene or an Olea europaea fruit extract titrated in maslinic and/or oleanolic acid. The delivery and release system may be contained in a cosmetic composition to be applied to skin, scalp, eyelashes, eyebrows, and nails.